Department of Chemistry, MS 015, Brandeis University, Waltham, MA 02454-9110, USA.
Adv Healthc Mater. 2013 Dec;2(12):1586-90. doi: 10.1002/adhm.201300041. Epub 2013 Apr 25.
None of the clinical trials of anti-HIV gels based on conventional polymers or lipid emulsions has been successful, suggesting the need of new molecular design of the anti-HIV gels. This paper reports the conversion of anti-HIV prodrugs into self-delivery supramolecular hydrogels. By covalently conjugating reverse transcriptase inhibitors to a versatile self-assembly motif, the hydrogelators that self-assemble to form supramolecular nanofibers as the matrices of hydrogels in a weak acidic condition are obtained. Upon the treatment of prostate acid phosphatase (PAP), the hydrogels exhibit drastically enhanced elasticity. The hydrogelators are biocompatible and able to release the inhibitors under physiological condition. The use of the self-assembly motif as a self-delivery agent containing non-steroid anti-inflammatory drug (NSAID) renders this hydrogel to be both anti-inflammatory and anti-HIV. This work illustrates an unprecedented approach for designing multifunctional supramolecular hydrogels that may serve as potential anti-HIV hydrogels for sustained drug release.
基于传统聚合物或脂乳的抗 HIV 凝胶的临床试验均未成功,这表明需要对抗 HIV 凝胶进行新的分子设计。本文报道了将抗 HIV 前药转化为自传递超分子水凝胶。通过将逆转录酶抑制剂共价连接到多功能自组装基序上,得到了在弱酸性条件下自组装形成超分子纳米纤维作为水凝胶基质的水凝胶剂。经前列腺酸性磷酸酶 (PAP) 处理后,水凝胶表现出显著增强的弹性。水凝胶剂具有生物相容性,并能在生理条件下释放抑制剂。将自组装基序用作包含非甾体抗炎药 (NSAID) 的自传递剂,使这种水凝胶具有抗炎和抗 HIV 的双重作用。这项工作展示了一种设计多功能超分子水凝胶的前所未有的方法,这种水凝胶可能作为用于持续药物释放的潜在抗 HIV 水凝胶。